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The role of cellular accumulation in determining sensitivity to platinum-based chemotherapy.
Annual Review of Pharmacology and Toxicology ( IF 11.2 ) Pub Date : 2007-10-17 , DOI: 10.1146/annurev.pharmtox.48.080907.180426
Matthew D Hall 1 , Mitsunori Okabe , Ding-Wu Shen , Xing-Jie Liang , Michael M Gottesman
Affiliation  

The platinum (Pt) drugs cisplatin and carboplatin are heavily employed in chemotherapy regimens; however, similar to other classes of drugs, a number of intrinsic and acquired resistance mechanisms hamper their effectiveness. The method by which Pt drugs enter cells has traditionally been attributed to simple passive diffusion. However, recent evidence suggests a number of active uptake and efflux mechanisms are at play, and altered regulation of these transporters is responsible for the reduced accumulation of drug in resistant cells. This review suggests a model that helps reconcile the disparate literature by describing multiple pathways for Pt-containing drugs into and out of the cell.

中文翻译:

细胞积累在确定对铂类化学疗法敏感性中的作用。

铂(Pt)药物顺铂和卡铂在化疗方案中大量使用;但是,与其他类别的药物类似,许多内在的和获得性的耐药机制也阻碍了它们的有效性。传统上将Pt药物进入细胞的方法归因于简单的被动扩散。但是,最近的证据表明,许多主动的吸收和外排机制正在发挥作用,而这些转运蛋白的调节改变导致耐药细胞中药物的积累减少。这篇综述提出了一个模型,该模型通过描述含Pt药物进出细胞的多种途径来帮助调和不同的文献。
更新日期:2019-11-01
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